A Phase 1 First‐in‐Human Single‐Ascending‐Dose Trial With ESB1609, a Selective Agonist to the Sphingosine‐1‐Phosphate Receptor 5
Sign Up to like & getrecommendations! Published in 2023 at "Clinical Pharmacology in Drug Development"
DOI: 10.1002/cpdd.1256
Abstract: ESB1609 is a small‐molecule sphingosine‐1‐phosphate‐5 receptor–selective agonist designed to restore lipid homeostasis by promoting cytosolic egress of sphingosine‐1‐phosphate to reduce abnormal levels of ceramide and cholesterol in disease. A phase 1 study was conducted in… read more here.
Keywords: csf; esb1609; phosphate receptor; sphingosine ... See more keywords
Cardiac Safety of Ozanimod, a Novel Sphingosine‐1‐Phosphate Receptor Modulator: Results of a Thorough QT/QTc Study
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DOI: 10.1002/cpdd.383
Abstract: Ozanimod is a novel, selective, oral sphingosine‐1‐phosphate (1 and 5) receptor modulator in development for multiple sclerosis and inflammatory bowel disease. This randomized, double‐blind, placebo‐controlled, positive‐controlled, parallel‐group thorough QT study characterized the effects of ozanimod… read more here.
Keywords: cardiac safety; sphingosine phosphate; phosphate receptor; receptor modulator ... See more keywords
Activation mechanisms of the first sphingosine‐1‐phosphate receptor
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DOI: 10.1002/pro.3165
Abstract: Activation of the first sphingosine‐1‐phosphate receptor (S1PR1) promotes permeability of the blood brain barrier, astrocyte and neuronal protection, and lymphocyte egress from secondary lymphoid tissues. Although an agonist often activates the S1PR1, the receptor exhibits… read more here.
Keywords: first sphingosine; activation mechanisms; sphingosine phosphate; activation ... See more keywords
Benefit–Risk Profile of Sphingosine-1-Phosphate Receptor Modulators in Relapsing and Secondary Progressive Multiple Sclerosis
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DOI: 10.1007/s40265-017-0814-1
Abstract: Since the approval of fingolimod, several selective sphingosine-1-phosphate receptor modulators have entered clinical development for multiple sclerosis. However, side effects can occur with sphingosine-1-phosphate receptor modulators. By considering short-term data across the drug class and… read more here.
Keywords: sphingosine phosphate; phosphate receptor; term; receptor modulators ... See more keywords
Mechanisms of sphingosine 1-phosphate receptor signalling in cancer.
Sign Up to like & getrecommendations! Published in 2017 at "Cellular signalling"
DOI: 10.1016/j.cellsig.2017.03.002
Abstract: S1P is a small bioactive lipid which exerts its effects following binding to a family of five G protein-coupled receptors, known as S1P1-5. Following receptor activation, multiple signalling cascades are activated, allowing S1P to regulate… read more here.
Keywords: phosphate receptor; s1prs; sphingosine phosphate; cancer ... See more keywords
Sphingosine-1-phosphate receptor therapies: Advances in clinical trials for CNS-related diseases
Sign Up to like & getrecommendations! Published in 2017 at "Neuropharmacology"
DOI: 10.1016/j.neuropharm.2016.11.006
Abstract: ABSTRACT The family of sphingosine‐1‐phosphate receptors (S1PRs) are G protein‐coupled and comprise of five subtypes, S1P1‐S1P5. These receptors are activated by the sphingolipid ligand, S1P, which is produced from the phosphorylation of sphingosine by sphingosine… read more here.
Keywords: sphingosine phosphate; clinical trials; related diseases; phosphate receptor ... See more keywords
Discovery of a Promising Fluorine-18 Positron Emission Tomography Radiotracer for Imaging Sphingosine-1-Phosphate Receptor 1 in the Brain.
Sign Up to like & getrecommendations! Published in 2023 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.2c01752
Abstract: Sphingosine-1-phosphate receptor 1 (S1PR1) is recognized as a novel therapeutic and diagnostic target in neurological disorders. We recently transferred the S1PR1 radioligand [11C]CS1P1 into clinical investigation for multiple sclerosis. Herein, we reported the design, synthesis… read more here.
Keywords: positron emission; brain; phosphate receptor; emission tomography ... See more keywords
Modulators of Sphingosine-1-phosphate Pathway Biology: Recent Advances of Sphingosine-1-phosphate Receptor 1 (S1P1) Agonists and Future Perspectives.
Sign Up to like & getrecommendations! Published in 2017 at "Journal of medicinal chemistry"
DOI: 10.1021/acs.jmedchem.6b01575
Abstract: The sphingoid base derived class of lipids (sphingolipids) is a family of interconverting molecules that play key roles in numerous structural and signaling processes. The biosynthetic pathway of the sphingolipids affords many opportunities for therapeutic… read more here.
Keywords: biology; receptor s1p1; s1p1 agonists; sphingosine phosphate ... See more keywords
Endothelial‐protective effects of a G‐protein‐biased sphingosine‐1 phosphate receptor‐1 agonist, SAR247799, in type‐2 diabetes rats and a randomized placebo‐controlled patient trial
Sign Up to like & getrecommendations! Published in 2020 at "British Journal of Clinical Pharmacology"
DOI: 10.1111/bcp.14632
Abstract: SAR247799 is a G‐protein‐biased sphingosine‐1 phosphate receptor‐1 (S1P1) agonist designed to activate endothelial S1P1 and provide endothelial‐protective properties, while limiting S1P1 desensitization and consequent lymphocyte‐count reduction associated with higher doses. The aim was to show… read more here.
Keywords: endothelial protective; biased sphingosine; sar247799; sphingosine phosphate ... See more keywords
Abstract 839: Sphingosine 1-Phosphate Receptor 1 in Cardiomyocytes Protects Against Cardiac Fibrosis
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DOI: 10.1161/res.125.suppl_1.839
Abstract: Sphingosine 1-phosphate receptor 1 (S1P 1 , encoded by S1pr1 ) is a G protein-coupled receptor that binds the ligand S1P and signals in multiple cell types including endothelium and cardiomyocytes. We previously demonstrated that… read more here.
Keywords: sphingosine phosphate; cardiac fibrosis; phosphate receptor; fibrosis ... See more keywords
Development and characterization of sphingosine 1-phosphate receptor 1 monoclonal antibody suitable for cell imaging and biochemical studies of endogenous receptors
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DOI: 10.1371/journal.pone.0213203
Abstract: Although sphingosine-1-phosphate receptor 1 (S1P1) has been shown to trigger several S1P targeted functions such as immune cell trafficking, cell proliferation, migration, or angiogenesis, tools that allow the accurate detection of endogenous S1P1 localization and… read more here.
Keywords: antibody; sphingosine phosphate; receptor; cell ... See more keywords